米库氯铵 | 133814-19-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异喹啉及其衍生物
• 中文名称: 米库氯铵
• 中文别名: 美维松
• 英文名称: Mivacurium
• 英文别名: bis[3-[(1R)-6,7-dimethoxy-2-methyl-1-[(3,4,5-trimethoxyphenyl)methyl]-3,4-dihydro-1H-isoquinolin-2-ium-2-yl]propyl] (E)-oct-4-enedioate
• CAS: 133814-19-4
• 化学式: C58H80N2O14+2
• 分子量: 1029.3
• InChiKey: ILVYCEVXHALBSC-OTBYEXOQSA-N

物化性质

• 物理描述：
  Liquid
• 溶解度：
  3.26e-05 g/L

计算性质

• 辛醇/水分配系数(LogP)：
  8.7
• 重原子数：
  74
• 可旋转键数：
  30
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  145
• 氢给体数：
  0
• 氢受体数：
  14

ADMET

代谢

通过血浆胆碱酯酶催化的酶促水解广泛且迅速进行。在血浆胆碱酯酶活性异常或降低的患者中，生物转化可能会显著减慢，尤其是那些具有纯合子非典型胆碱酯酶基因异常的个体。

Extensive and rapid via enzymatic hydrolysis catalyzed by plasma cholinesterase. Biotransformation may be significantly slowed in patients with abnormal or decreased plasma cholinesterase activity, especially individuals with a homozygous atypical cholinesterase gene abnormality.

来源:DrugBank

毒理性

• 药物性肝损伤

混合物：米伐库林

Compound:mivacurium

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

毒理性

• 药物性肝损伤

DILI 注释：无 DILI（药物性肝损伤）担忧

DILI Annotation:No-DILI-Concern

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

毒理性

• 药物性肝损伤

标签部分：无匹配

Label Section:No match

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

毒理性

• 药物性肝损伤

参考文献：M Chen, V Vijay, Q Shi, Z Liu, H Fang, W Tong. 美国食品药品监督管理局批准的药物标签用于研究药物诱导的肝损伤，《药物发现今日》，16(15-16):697-703, 2011. PMID:21624500 DOI:10.1016/j.drudis.2011.05.007 M Chen, A Suzuki, S Thakkar, K Yu, C Hu, W Tong. DILIrank：按人类发展药物诱导肝损伤风险排名的最大参考药物清单。《药物发现今日》2016, 21(4): 648-653. PMID:26948801 DOI:10.1016/j.drudis.2016.02.015

References:M Chen, V Vijay, Q Shi, Z Liu, H Fang, W Tong. FDA-Approved Drug Labeling for the Study of Drug-Induced Liver Injury, Drug Discovery Today, 16(15-16):697-703, 2011. PMID:21624500 DOI:10.1016/j.drudis.2011.05.007 M Chen, A Suzuki, S Thakkar, K Yu, C Hu, W Tong. DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. Drug Discov Today 2016, 21(4): 648-653. PMID:26948801 DOI:10.1016/j.drudis.2016.02.015

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

毒理性

• 蛋白质结合

米瓦库林由于被血浆胆碱酯酶迅速水解，其蛋白质结合尚未确定。

The protein binding of mivacurium has not been determined due to its rapid hydrolysis by plasma cholinesterase.

来源:DrugBank

文献信息

• Active agent delivery systems and methods for protecting and administering active agents
  申请人：Mickle Travis

  公开号：US20070232529A1

  公开（公告）日：2007-10-04

  The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents and methods for administering conjugated active agent compositions.

  本发明涉及活性物质输送系统，更具体地涉及包含氨基酸（作为单个氨基酸或肽）与活性物质共价连接的组合物以及用于给予共轭活性物质组合物的方法。
• Process for the preparation of mivacurium chloride
  申请人：Velati Maurizio Francesco

  公开号：US20070293534A1

  公开（公告）日：2007-12-20

  A process for preparing the [R-[R*,R*-(E)]]- 2,2 ′-( 1,8 -dioxo- 4 -octene- 1,8 -diyl) bis(oxy- 3,1 -propanediyl)bis( 1,2,3,4 -tetrahydro- 6,7 -dimethoxy- 2 -methyl- 1 -[( 3,4,5 -trimethoxyphenyl) methyl]isoquinolinium) dichloride, commonly known as mivacurium chloride, useful as short-duration neuromuscular blocking agent.

  一种制备[R-[R*，R*-(E)]]-2,2′-(1,8-二氧代-4-辛烯-1,8-二基)双(氧-3,1-丙二醇基)双(1,2,3,4-四氢-6,7-二甲氧基-2-甲基-1-[(3,4,5-三甲氧基苯基)甲基]异喹啉)二氯化物的工艺，通常称为米瓦库溴化物，用作短效神经肌肉阻滞剂。
• INTERMEDIATE DURATION NEUROMUSCULAR BLOCKING AGENTS AND ANTAGONISTS THEREOF
  申请人：Savarese John J.

  公开号：US20080139482A1

  公开（公告）日：2008-06-12

  The invention provides novel neuromuscular blocking agents, methods of using the neuromuscular blocking agents as well as reagents, methods and kits for reversing the effects of the neuromuscular blocking agents.
• ACYCLIC CUCURBIT[N]URIL TYPE MOLECULAR CONTAINERS TO TREAT INTOXICATION AND DECREASE RELAPSE RATE IN SUBSTANCE ABUSE DISORDERS
  申请人：UNIVERSITY OF MARYLAND, COLLEGE PARK

  公开号：US20170246180A1

  公开（公告）日：2017-08-31

  Provided are methods for reversing the effects of drugs of abuse. The method involves administering acyclic CB[n]-type compounds to a mammal in need of the reversal of the effects from a drug of abuse.
• US4761418A
  申请人：——

  公开号：US4761418A

  公开（公告）日：1988-08-02